Propylthiouracil (PTU) pharmacology in the rat. I. Serum and thyroid PTU measurements by radioimmunoassay.

Abstract:

:We have developed a highly sensitive and specific RIA for propylthiouracil (PTU) which uses 125I-labeled PTU as the radioactive ligand. At a final antibody dilution of 1:10,000, the detection limit for PTU was 100 pg; cross-reactivity with circulating, urinary, and intrathyroid PTU metabolites was negligible. Using this assay, serum and thyroid PTU levels were determined after short term (1 week) and long term (1 month) PTU treatment at doses of 0.0001-0.05%. Serum PTU was a linear function of the PTU dose (r = 0.99; P less than 0.001), whereas thyroid PTU was a linear function of the logarithm of the PTU dose (r = 0.99; P less than 0.001). Serum PTU levels were higher after 1 month of treatment than after administration for 1 week, probably because steady state conditions were not achieved after 1 week. At several doses, thyroid PTU levels were also higher after 1 month of treatment, but the differences were not as striking as those seen in the serum levels. The pharmacokinetic data are consistent with a multicompartmental model for PTU distribution. The logarithmic relationship between thyroid PTU and PTU dose suggests a saturable uptake mechanism for PTU by the thyroid; inhibition of thyroid PTU uptake by PTU itself could also explain these observations.

journal_name

Endocrinology

journal_title

Endocrinology

authors

Halpern R,Cooper DS,Kieffer JD,Saxe V,Mover H,Maloof F,Ridgway EC

doi

10.1210/endo-113-3-915

subject

Has Abstract

pub_date

1983-09-01 00:00:00

pages

915-20

issue

3

eissn

0013-7227

issn

1945-7170

journal_volume

113

pub_type

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